An antibiotic agent is a drug that kills bacteria or slows their growth. Antibiotics are relatively harmless to the host, and therefore can be used to treat infections.
Antibiotics can be administered in a variety of ways, including orally, intravenously and topically.
There are relatively few classes of antibiotics currently available to treat bacterial infections. Several of the known antibiotics have significant side effects, such as dangerous allergic reactions or inconvenient gastrointestinal disturbances (see Table 1).
TABLE 1Existing classes of antibiotics and their known side effects.ClassAntibiotic Generic NameKnown Side EffectsAminoglycosidesAmikacin; Gentamicin; Kanamycin;Hearing lossNeomycin; Netilmicin; Streptomycin;VertigoTobramycinKidney damageCarbacephemLoracarbefCarbapenemsErtapenem; Imipenem/Cilastatin;MeropenemCephalosporinsCefadroxil; Cefazolin; Cephalexin;Gastrointestinal upset and(First, second, thirdCefaclor; Cefamandole; CefoxitinCefprozil;diarrheaand fourthCefuroxime; Cefixime; Cefdinir; Cefditoren;Nausea (if alcohol takengenerations)Cefoperazone; Cefotaxime; Cefpodoxime;concurrently)Ceftazidime; Ceftibuten; Ceftizoxime;Allergic reactionsCeftriaxone; Cefepime;GlycopeptidesVancomycin;MacrolidesAzithromycin; Clarithromycin;Dirithromycin; Erythromycin;Roxithromycin; TroleandomycinMonobactamAztreonam;PenicillinsAmoxicillin; Ampicillin; Azlocillin;Gastrointestinal upset andCarbenicillin; Cloxacillin; Dicloxacillin;diarrheaFlucloxacillin; Mezlocillin; Nafcillin;Allergy with serious anaphylacticPenicillin; Piperacillin; TicarcillinreactionsBrain and kidney damagePolypeptidesBacitracin; Colistin; Polymyxin; BKidney and nerve damage (whengiven by injection)QuinolonesCiprofloxacin; Enoxacin; Gatifloxacin;NauseaLevofloxacin; Lomefloxacin; Moxifloxacin;Norfloxacin; Ofloxacin; Trovafloxacin;SulfonamidesMafenide; Prontosil (archaic);Nausea, vomiting, and diarrheaSulfacetamide; Sulfamethizole;Allergy (including skin rashes)Sulfanilimide (archaic); Sulfasalazine;Crystals in urineSulfisoxazole; Trimethoprim; Trimethoprim-Kidney failureSulfamethoxazole (Co-trimoxazole) (TMP-Decrease in white blood cell countSMX)Sensitivity to sunlightTetracyclinesDemeclocycline; Doxycycline; Minocycline;Gastrointestinal upsetOxytetracycline; TetracyclineSensitivity to sunlightStaining of teethPotential toxicity to mother andfetus during pregnancyOthersChloramphenicol; Clindamycin;Ethambutol; Fosfomycin; Furazolidone;Isoniazid; Linezolid; Metronidazole;Nitrofurantoin; Platensimycin;Pyrazinamide; Guinupristin/Dalfopristin;Rifampin; Spectinomycin
All antibiotics have a certain delimited spectrum of action. This spectrum of action can sometimes be very narrow. For example, antibiotics activity can be limited to gram-positive or gram-negative bacteria.
In consequence, there are only a limited number of antibiotics that can be used for treating any given infection. Faced with this limited choice, physicians are sometimes forced to prescribe antibiotics having side effects.
There are also serious concerns about strains of bacteria developing antibiotic resistance making them untreatable by any available antibiotics. Indeed, one of the most frequent problems in hospital is the presence of bacteria resistant to the most common antibiotic agents. One such resistant strain of bacteria is methicillin-resistant Staphylococcus aureus (MRSA). MRSA is a bacterium responsible for difficult-to-treat infections in humans. It may also be referred to as multiple-resistant Staphylococcus aureus or oxacillin-resistant Staphylococcus aureus (ORSA). MRSA is a resistant variation of the common bacterium Staphylococcus aureus. It has evolved an ability to survive treatment with beta-lactam antibiotics, including penicillin, methicillin, and cephalosporins. MRSA is especially troublesome in hospital-associated (nosocomial) infections. In hospitals, patients with open wounds, invasive devices, and weakened immune systems are at greater risk for infection than the general public. Hospital staff that does not follow proper sanitary procedures may transfer bacteria from patient to patient. MRSA is now found worldwide. MRSA is often referred to in the press as a “superbug.” In the past decade or so the number of MRSA infections in the United States has increased significantly. Some published figures suggest that MRSA infections are responsible for more deaths in the U.S. each year than AIDS. Vancomycin is the latest treatment now used for treating MRSA, but new strains of Staphylococcus aureus presenting a resistance to vancomycin (VRSA) are now appearing.
There is therefore a need for new chemical compounds having antibiotic properties. The present invention therefore aims to provide such compounds.
The present description refers to a number of documents, the content of which is herein incorporated by reference in their entirety.